Development and validation of an HPLC-MS/MS method to quantify the KRAS inhibitor adagrasib in mouse plasma and tissue-related matrices

Article Oncology

First-in-Human Phase I/IB Dose-Finding Study of Adagrasib (MRTX849) in Patients With Advanced KRASG12C Solid Tumors (KRYSTAL-1)

Sai-Hong Ignatius Ou et al.

Summary: This study reported the results of a clinical trial using adagrasib to treat non-small-cell lung cancer, colorectal cancer, and other solid tumors with the KRAS(G12C) mutation. The recommended phase II dose was identified as 600 mg twice a day, and it demonstrated good tolerability and antitumor activity.

JOURNAL OF CLINICAL ONCOLOGY (2022)

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Article Chemistry, Analytical

Development and validation of a robust and sensitive HPLC-MS/MS method for the quantitation of MRTX849 in plasma and its application in pharmacokinetics

Ping Du et al.

Summary: MRTX849 is a novel targeted inhibitor of KRAS (G12C) that improves the response rate in patients with advanced solid tumors. This study reports an analytical HPLC-MS/MS assay and pharmacokinetics for MRTX849 in plasma, demonstrating the accuracy and validity of the method.

ANALYST (2022)

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Article Biochemical Research Methods

Validated HPLC-MS/MS method for quantitation of AMG 510, a KRAS G12C inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice

Naveena Madhyastha et al.

Summary: AMG 510, the first-in-class KRAS(G12C) inhibitor, is currently in phase 2 clinical trials for treating non-small cell lung cancer patients. A sensitive, selective, and high-throughput HPLC-MS/MS method was developed and validated for the quantitation of AMG 510 in mouse plasma, and successfully applied in a pharmacokinetic study in mice.

BIOMEDICAL CHROMATOGRAPHY (2021)

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Article Oncology